JP5116092B2 - プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物 - Google Patents

プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物 Download PDF

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JP5116092B2
JP5116092B2 JP2007532549A JP2007532549A JP5116092B2 JP 5116092 B2 JP5116092 B2 JP 5116092B2 JP 2007532549 A JP2007532549 A JP 2007532549A JP 2007532549 A JP2007532549 A JP 2007532549A JP 5116092 B2 JP5116092 B2 JP 5116092B2
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aliphatic
substituted
optionally substituted
compound
optionally
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JP2008513488A5 (pl
JP2008513488A (ja
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フランチェスコ ジー. サリトゥロ,
マーク ダブリュー. レデボーア,
ブライアン レッドフォード,
チァン ワン,
アルバート シー. ピアース,
ジョン ピー. ダフィ,
デイビッド メッサースミス,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2007532549A 2004-09-17 2005-09-19 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物 Expired - Fee Related JP5116092B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US61090204P 2004-09-17 2004-09-17
US60/610,902 2004-09-17
PCT/US2005/033333 WO2006034116A1 (en) 2004-09-17 2005-09-19 Diaminotriazole compounds useful as protein kinase inhibitors

Related Child Applications (1)

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JP2008222676A Division JP2009019048A (ja) 2004-09-17 2008-08-29 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物

Publications (3)

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JP2008513488A JP2008513488A (ja) 2008-05-01
JP2008513488A5 JP2008513488A5 (pl) 2008-10-16
JP5116092B2 true JP5116092B2 (ja) 2013-01-09

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JP2007532549A Expired - Fee Related JP5116092B2 (ja) 2004-09-17 2005-09-19 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物
JP2008222676A Withdrawn JP2009019048A (ja) 2004-09-17 2008-08-29 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物
JP2013024247A Pending JP2013082756A (ja) 2004-09-17 2013-02-12 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物

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JP2008222676A Withdrawn JP2009019048A (ja) 2004-09-17 2008-08-29 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物
JP2013024247A Pending JP2013082756A (ja) 2004-09-17 2013-02-12 プロテインキナーゼの阻害剤として有用なジアミノトリアゾール化合物

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US (1) US7329652B2 (pl)
EP (1) EP1791830B1 (pl)
JP (3) JP5116092B2 (pl)
KR (1) KR20070057955A (pl)
CN (1) CN101039933B (pl)
AT (1) ATE493401T1 (pl)
AU (1) AU2005286968A1 (pl)
CA (1) CA2580610C (pl)
CY (1) CY1112253T1 (pl)
DE (1) DE602005025655D1 (pl)
DK (1) DK1791830T3 (pl)
ES (1) ES2359007T3 (pl)
IL (1) IL181987A0 (pl)
MX (1) MX2007003154A (pl)
NO (1) NO20071915L (pl)
NZ (1) NZ580450A (pl)
PL (1) PL1791830T3 (pl)
PT (1) PT1791830E (pl)
RU (1) RU2443700C2 (pl)
SI (1) SI1791830T1 (pl)
WO (1) WO2006034116A1 (pl)
ZA (1) ZA200702645B (pl)

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RS53281B (sr) * 2006-12-29 2014-08-29 Rigel Pharmaceuticals Inc. Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori
AU2016259396B2 (en) * 2006-12-29 2018-11-08 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as Axl inhibitors
CA2710051C (en) 2006-12-29 2017-05-16 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
AU2014200824B2 (en) * 2006-12-29 2016-12-15 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as Axl inhibitors
CN101622248B (zh) 2006-12-29 2013-04-17 里格尔制药公司 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑
CA2710230C (en) * 2006-12-29 2016-02-23 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
BRPI0813356A2 (pt) * 2007-06-15 2014-12-30 Irm Llc Inibidores de proteína quinase e métodos para uso dos mesmos
JP2011500625A (ja) * 2007-10-18 2011-01-06 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ トリ置換された1,2,4−トリアゾール
JO2784B1 (en) * 2007-10-18 2014-03-15 شركة جانسين فارماسوتيكا ان. في 5,3,1 - Triazole substitute derivative
CA2704052C (en) 2007-10-26 2015-04-21 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
AR070936A1 (es) * 2008-03-19 2010-05-12 Janssen Pharmaceutica Nv 1,2,4 -triazoles trisustituidos
JP5486591B2 (ja) * 2008-05-09 2014-05-07 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ アセチルコリン受容体モジュレーターとしての三置換ピラゾール
CA2730251C (en) 2008-07-09 2016-08-09 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
BRPI1007046B1 (pt) 2009-01-16 2019-07-16 Rigel Pharmaceuticals, Inc. Inibidores axl para uso em terapia de combinação para evitar, tratar ou controlar o câncer metastático.
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WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
RS62649B1 (sr) 2013-03-12 2021-12-31 Vertex Pharma Inhibitori dnk-pk
KR102411227B1 (ko) 2013-10-17 2022-06-21 버텍스 파마슈티칼스 인코포레이티드 Dna-pk 억제제로서 (s)-n-메틸-8-(1-((2'-메틸-[4,5'-비피리미딘]-6-일)아미노)프로판-2-일)퀴놀린-4-카복스아미드 및 이의 듀테로화된 유도체의 공결정
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
MX394860B (es) 2016-09-27 2025-03-24 Vertex Pharma Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk).
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2020201362A2 (en) 2019-04-02 2020-10-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
KR102133595B1 (ko) 2019-05-31 2020-07-13 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
KR102112336B1 (ko) 2019-08-12 2020-05-18 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation
WO2026093435A1 (en) 2024-10-31 2026-05-07 Institut National de la Santé et de la Recherche Médicale Use of jak inhibitors for enhancing the potency of immunotherapy in the treament of cancer

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SI1791830T1 (sl) 2011-05-31
NO20071915L (no) 2007-05-18
KR20070057955A (ko) 2007-06-07
US7329652B2 (en) 2008-02-12
PT1791830E (pt) 2011-04-04
JP2009019048A (ja) 2009-01-29
CA2580610A1 (en) 2006-03-30
CN101039933A (zh) 2007-09-19
CA2580610C (en) 2013-07-09
NZ580450A (en) 2011-06-30
ES2359007T3 (es) 2011-05-17
WO2006034116A1 (en) 2006-03-30
MX2007003154A (es) 2007-05-15
RU2007114293A (ru) 2008-10-27
PL1791830T3 (pl) 2011-05-31
EP1791830B1 (en) 2010-12-29
ZA200702645B (en) 2008-08-27
AU2005286968A1 (en) 2006-03-30
US20060063756A1 (en) 2006-03-23
DK1791830T3 (da) 2011-04-18
DE602005025655D1 (de) 2011-02-10
EP1791830A1 (en) 2007-06-06
CN101039933B (zh) 2012-06-06
IL181987A0 (en) 2007-07-04
JP2008513488A (ja) 2008-05-01
JP2013082756A (ja) 2013-05-09
CY1112253T1 (el) 2015-12-09
RU2443700C2 (ru) 2012-02-27
ATE493401T1 (de) 2011-01-15

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